Eudragit RL-based film coatings: How to minimize sticking and adjust drug release using MAS

Eur J Pharm Biopharm. 2020 Mar:148:126-133. doi: 10.1016/j.ejpb.2020.01.011. Epub 2020 Jan 23.

Abstract

Polymeric film coatings based on quaternary polymethacrylates (QPMs, e.g. Eudragits®) are frequently used for controlled release applications. However, their considerable sticking tendency is a major drawback in practice. In this study, different amounts of magnesium aluminum silicate (MAS) were added to the film coatings in order to overcome this hurdle. MAS is negatively charged and can electrostatically interact with the positively charged QPM. Different types of tablet cores were coated with aqueous Eudragit® RL 30D dispersions, optionally containing varying amounts of MAS. Dynamic changes in the wet mass of the systems as well as drug release upon exposure to 0.1 M HCl and phosphate buffer pH 6.8 were monitored. Propranolol HCl, acetaminophen, and diclofenac sodium were used as cationic, nonionic and anionic model drugs. The tablets were optionally cured for 12 h at 45 or 60 °C. Importantly, the addition of MAS to aqueous Eudragit® RL 30D dispersion substantially reduced the films' stickiness and led to stable inner coating structures, even without curing. Desired drug release rates can be adjusted by varying the QPM:MAS ratio and coating level.

Keywords: Drug release; Eudragit RL; Magnesium aluminum silicate; Quaternary polymethacrylate; Tablet coating.

MeSH terms

  • Acetaminophen / chemistry
  • Aluminum Compounds / chemistry*
  • Chemistry, Pharmaceutical
  • Delayed-Action Preparations
  • Diclofenac / chemistry
  • Drug Liberation
  • Excipients / chemistry*
  • Magnesium Compounds / chemistry*
  • Polymers / chemistry*
  • Propranolol / chemistry
  • Silicates / chemistry*
  • Tablets
  • Temperature

Substances

  • Aluminum Compounds
  • Delayed-Action Preparations
  • Excipients
  • Magnesium Compounds
  • Polymers
  • Silicates
  • Tablets
  • Diclofenac
  • Acetaminophen
  • Eudragit RL
  • aluminum magnesium silicate
  • Propranolol